相似化合物
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2-chloro-5-trifluoromethylpyridine piperazine 2-bromo-5-(trifluoromethyl)pyridine 2-methyl-2-[4-(5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-propionic acid 4-[4-(5-Trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-benzoic acid tert-butyl ester (2R)-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}propanoic acid 📜2-溴-5-(三氟甲基)吡啶置于tris-(Dibenzylideneacetone)Dipalladium(0),R-(+)-1,1'-联萘-2,2'-双二苯膦,三氟乙酸,Sodium T-Butanolate体系中,用 二氯甲烷,甲苯 用作溶剂,化学反应 15.0H,反应生成1-[5-(三氟甲基)-2-吡啶基]哌嗪
参考文献:具有混合结构的新型苯甘氨酰胺衍生物可作为新型广谱抗惊厥药的候选者
标题:具有混合结构的新型苯甘氨酰胺衍生物可作为新型广谱抗惊厥药的候选者
摘要:在本研究中,应用集中的组合化学方法将众所周知的 Trpv1 拮抗剂的结构片段与我们小组先前发现的强效抗惊厥先导化合物ka-104合并.因此,在体内和体外试验中设计,合成和表征了一系列 22 种原始化合物.获得的化合物在最大电击 (Mes) 测试和 6 Hz 癫痫模型(使用 32 和 44 Ma 电流强度)中显示出强大的体内抗癫痫活性.最有效的化合物53和60显示出以下药理学特征:Ed 50 = 89.7 Mg/kg (Mes),Ed 50 = 29.9 Mg/kg (6 Hz,32 Ma),Ed 50= 68.0 Mg/kg (6 Hz,44 Ma),Ed 50 = 73.6 Mg/kg (Mes),Ed 50 = 24.6 Mg/kg (6 Hz,32 Ma),Ed 50 = 56.3 Mg/kg (6赫兹,44毫安),分别.此外,53和60对iv Ptz 癫痫发作阈值有效,
Doi:10.3390/cells11121862
海关参考信息
- 2921211000-乙二胺
2933310010-吡啶
2903399090-其他无环烃卤化衍生物
2939800000-其他生物碱 - 💡 提示:海关信息按照顺序优先匹配,如需确认的海关信息,请参考相关资料。
- 详情请参考:📖 海关编码查询和海关进出口税则
专利信息
专利号:US-2015239796-A1
优先权日:2014-02-19
标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane
发明人:RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS
权利人:UNIV OSLO
摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).
专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人:BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
专利号:US-9676721-B2
优先权日:2010-09-03
标题 :Compounds and compositions for the inhibition of NAMPT
发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
专利号:US-9555039-B2
优先权日:2011-05-09
标题:Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (NAMPT)
发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
权利人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)
专利号:US-9169209-B2
优先权日:2011-05-04
标题:Compounds and compositions for the inhibition of NAMPT
发明人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
权利人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
摘要:The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
专利号:US-8318928-B2
优先权日:2008-12-15
标题 :Fused imidazole carboxamides as TRPV3 modulators
发明人:CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
权利人:CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI; GLENMARK PHARMACEUTICALS SA
摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.